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PubMedDate not supplied

Oxidation of aldose reductase inhibitors ALO-4114 and ALO-3152 catalyzed by liver microsomes.

Rat and Cynomolgus monkey liver microsomes catalyze the oxidation of 2.7-difluoro-4.5-dimethoxyspiro (9H-fluorene-9,4'-imidazolidine)-2',5'-dione (ALO-4114) to its monomethoxymetabolite (ALO-4417). Formation of this product by O-demethylation of ALO-4114 is catalyzed by NADPH and oxygen-dependent microsomal enzymes with the properties of P-450 monooxygenases. The reaction is blocked by inhibitors selective for these enzymes and activity increases about 2-fold in rats pretreated with phenobarbital or methylcholanthrene. The increase in the O-demethylation of ALO-4114 was, however, considerably less than the increase in benzphetamine N-demethylation or nitrophenetole O-deethylation activities in liver microsomes from rats pretreated with either phenobarbital or methylcholanthrene. Rats pretreated with 20 or 40 mg/kg of ALO-4114 for 3-4 days failed to change significantly the rate of ALO-4114 O-demethylase activity of liver microsomes. O-Demethylation of the achiral ALO-4114 yields the chiral ALO-4417. The enantiomers separated on a Daicel Chiracel AS column by HPLC indicated that O-demethylation of ALO-4114 by microsomes from untreated rats was only slightly stereoselective. However, rats pretreated with methylcholanthrene not only enhanced activity, but also increased the formation of one enantiomer. Further oxidative metabolism of the enantiomers was slow and barely detectable in vitro. Studies conducted with Cynomolgus monkey liver microsomes from one male and one female per experimental group were generally consistent with those from the rat, but some differences were noted. Whether the differences are real or only reflect individual variations caused by the small sample size is not known at present.

Aldehyde Reductase↗
PubMed1995

The complete amino acid sequence of a mannose-binding lectin from "Kidachi Aloe" (Aloe arborescens Miller var. natalensis Berger).

The complete amino acid sequence of a mannose-binding lectin purified from the leaf skin of "Kidachi Aloe" (Aloe arborescens Miller var. natalensis Berger) is presented. The 109-residue sequence of the subunit was determined by analysis of peptides of the intact or S-pyridylethylated protein generated by digestion with cyanogen bromide, BNPS-skatole, Achromobacter protease I, or trypsin. The subunit contains an intrachain disulfide bridge. The sequence is highly homologous to that of a mannose-binding lectin from snowdrop bulb.

Aloe↗
PubMed1990

The stimulation of postdermabrasion wound healing with stabilized aloe vera gel-polyethylene oxide dressing.

Full-face dermabrasion provided an ideal opportunity to document the effects of dressings on wound healing management. Following the procedure, the abraded face was divided in half. One side was treated with the standard polyethylene oxide gel wound dressings. The other side was treated with a polyethylene oxide gel dressing saturated with stabilized aloe vera. The polyethylene oxide dressing provided an excellent matrix for the release of aloe vera gel during the initial 5 days of wound healing. By 24-48 hours there was dramatic vasoconstriction and accompanying reduction in edema on the aloe-treated side. By the third to fourth day there was less exudate and crusting at the aloe site, and by the fifth to sixth day the reepithelialization at the aloe site was complete. Overall, wound healing was approximately 72 hours faster at the aloe site. This acceleration in wound healing is important to reduce bacterial contamination, subsequent keloid formation, and/or pigmentary changes. The exact mechanism of acceleration of wound healing by aloe vera is unknown.

Aloe↗
PubMed1986

The antidiabetic activity of aloes: preliminary clinical and experimental observations.

The dried sap of the aloe plant (aloes) is one of several traditional remedies used for diabetes in the Arabian peninsula. Its ability to lower the blood glucose was studied in 5 patients with non-insulin-dependent diabetes and in Swiss albino mice made diabetic using alloxan. During the ingestion of aloes, half a teaspoonful daily for 4-14 weeks, the fasting serum glucose level fell in every patient from a mean of 273 +/- 25 (SE) to 151 +/- 23 mg/dl (p less than 0.05) with no change in body weight. In normal mice, both glibenclamide (10 mg/kg twice daily) and aloes (500 mg/kg twice daily) induced hypoglycaemia after 5 days, 71 +/- 6.2 and 91 +/- 7.6 mg/dl, respectively, versus 130 +/- 7 mg/dl in control animals (p less than 0.01); only glibenclamide was effective after 3 days. In the diabetic mice, fasting plasma glucose was significantly reduced by glibenclamide and aloes after 3 days. Thereafter only aloes was effective and by day 7 the plasma glucose was 394 +/- 22.0 versus 646 +/- 35.9 mg/dl, in the controls and 726 +/- 30.9 mg/dl in the glibenclamide treated group (p less than 0.01). We conclude that aloes contains a hypoglycaemic agent which lowers the blood glucose by as yet unknown mechanisms.

Aloe↗
PubMed1995

Treatment of experimental frostbite with pentoxifylline and aloe vera cream.

OBJECTIVE: To compare the therapeutic effects of systemic pentoxifylline and topical aloe vera cream in the treatment of frostbite. DESIGN: The frostbitten ears of 10 New Zealand white rabbits were assigned to one of four treatment groups: untreated controls, those treated with aloe vera cream, those treated with pentoxifylline, and those treated with aloe vera cream and pentoxifylline. MAIN OUTCOME MEASURES: Tissue survival was calculated as the percent of total frostbite area that remained after 2 weeks. RESULTS: The control group had a 6% tissue survival. Tissue survival was notably improved with pentoxifylline (20%), better with aloe vera cream (24%), and the best with the combination therapy (30%). CONCLUSION: Pentoxifylline is as effective as aloe vera cream in improving tissue survival after frostbite injury.

Administration, Topical↗
PubMed1990

Effect of aloes on blood glucose levels in normal and alloxan diabetic mice.

The acute and chronic effects of the exudate of Aloe barbadensis leaves and its bitter principle were studied on plasma glucose levels of alloxan-diabetic mice. Aloes was administered orally, 500 mg/kg, and the bitter principle was administered intraperitoneally, 5 mg/kg. The hypoglycemic effect of a single oral dose of aloes on serum glucose level was insignificant whereas that of the bitter principle was very highly significant and extended over a period of 24 h with maximum hypoglycemia observed at +8 h. In chronic studies, aloes was administered twice daily and the bitter principle was administered once a day for 4 days. The maximum reduction in plasma glucose level was observed at the 5th day in both cases. The hypoglycemic effect of aloes and its bitter principle may be mediated through stimulating synthesis and/or release of insulin from the beta-cells of Langerhans.

Administration, Oral↗
PubMed1988

Aloe vera.

We review the scientific literature regarding the aloe vera plant and its products. Aloe vera is known to contain several pharmacologically active ingredients, including a carboxypeptidase that inactivates bradykinin in vitro, salicylates, and a substance(s) that inhibits thromboxane formation in vivo. Scientific studies exist that support an antibacterial and antifungal effect for substance(s) in aloe vera. Studies and case reports provide support for the use of aloe vera in the treatment of radiation ulcers and stasis ulcers in man and burn and frostbite injuries in animals. The evidence for a potential beneficial effect associated with the use of aloe vera is sufficient to warrant the design and implementation of well-controlled clinical trials.

Aloe↗
PubMed1990

Studies of aloe. III. Mechanism of cathartic effect. (2).

The mechanism of action of aloe-emodin-9-anthrone, a decomposition product of barbaloin, in causing a significant increase in the water content of the rat large intestine, was investigated. Aloe-emodin-9-anthrone inhibited rat colonic Na+, K(+)-adenosine triphosphatase (ATPase) in vitro, and increased the paracellular permeability across the rat colonic mucosa in vivo. Therefore, it seemed that the increase in water content of the rat large intestine produced by aloe-emodin-9-anthrone was due to both inhibition of absorption and stimulation of secretion without stimulation of peristalsis. Furthermore, pretreatment with loperamide, an antidiarrheal agent, completely prevented the increase of paracellular permeability induced by aloe-emodin-9-anthrone but did not completely reduce the concomitant increase in residual fluid volume. These findings suggest that aloe-emodin-9-anthrone has multiple mechanisms of action involved in the increase of water content in the rat large intestine.

Aloe↗
PubMed1995

Effect of aloe vera gel to healing of burn wound a clinical and histologic study.

In a study of twenty-seven patients with partial thickness burn wound, they were treated with aloe vera gel compared with vaseline gauze. It revealed the aloe vera gel treated lesion healed faster than the vaseline gauze area. The average time of healing in the aloe gel area was 11.89 days and 18.19 days for the vaseline gauze treated wound. Statistical analysis by using t-test and the value of P < 0.002 was statistically significant. In histologic study, it showed early epithelialization in the treated aloe vera gel area. Only some minor adverse effects, such as discomfort and pain were encountered in the 27 cases. This study showed the effectiveness of aloe vera gel on a partial thickness burn wound, and it might be beneficial to do further trials on burn wounds.

Adolescent↗
PubMed1987

Effects of ALO 2145 on intraocular pressure following argon laser trabeculoplasty.

A prospective, randomized, double-masked study compared topical 1% ALO 2145, an alpha 2-agonist, with placebo in therapy for immediate postoperative intraocular pressure (IOP) rise after argon laser trabeculoplasty. Seventy-three eyes (73 patients) underwent 360 degrees of treatment utilizing 80 spots of 800 to 1000 mW of power. Intraocular pressure rise was measured hourly for the first three hours after operation, at one week, and at one month. Eyes treated with ALO 2145 had both significantly lower mean IOPs and greater IOP decreases from baseline than placebo-treated eyes during the first three hours after operation. No eyes treated with ALO 2145 and six eyes (18%) treated with placebo experienced an IOP rise of 10 mm Hg or greater. Twenty eyes (59%) in the placebo group and eight eyes (21%) treated with ALO 2145 had an IOP elevation. No change was detected in the mean heart rate. ALO 2145 appears to be effective in eliminating large, acute IOP elevations after argon laser trabeculoplasty.

Adrenergic alpha-Agonists↗
PubMed1988

ALO 2145 reduces the intraocular pressure elevation after anterior segment laser surgery.

The effect of an alpha adrenergic agonist, ALO 2145 (para-amino-clonidine [PAC]), was examined in a double-masked, multicenter study on the postoperative intraocular pressure (IOP) elevation after laser surgery in 165 patients (83 trabeculoplasty, 36 iridotomy, and 46 capsulotomy). One drop of 1.0% ALO 2145 or vehicle was instilled 1 hour before and immediately after laser surgery. The mean IOP increase in the ALO 2145-treated group was lower (P less than 0.05) than in the placebo group at each of the first three postoperative hours. Overall, 18% of placebo-treated eyes experienced IOP increases greater than or equal to 10 mmHg as compared with 4% of ALO 2145-treated eyes (P less than 0.003). Ocular and systemic side effects were minimal and did not differ between the treatment groups. ALO 2145 safely and effectively reduced the incidence and magnitude of potentially harmful IOP elevations after anterior segment laser surgery.

Aged↗
PubMed1992

[Efficacy and tolerability of apraclonidine (ALO 2145, 1%) in the prevention of early ocular hypertonia, after trabeculoretraction using argon laser and posterior capsulotomy using Nd:YAG laser].

ALO 2145 (Apraclonidine Chlorhydrate)*, is a new hypotensive agent; it acts as a selective alpha-2-adrenergic agonist to produce a marked reduction in intraocular pressure with minimal effect on the cardiovascular system. 38 patients undergoing ocular laser surgery were allocated to treatment with either ALO 2145 1% (n = 20), or to placebo (n = 18), in a double-masked fashion. One drop of study medication was instilled into the operative eye one hour before laser surgery, and one drop immediately after the laser surgery. ALO 2145 treated eyes exhibited a significantly lower mean intraocular pressure increase in the immediate postoperative phase, compared with placebo treated eyes. ALO 2145 also significantly reduced the postoperative incidence of intraocular pressure spikes, defined as intraocular pressure increases of more than 10 mmHg over baseline (17% of cases for active treatment vs 60% of cases for placebo). ALO 2145 1% was shown to be effective and well tolerated in the dosage regimen employed in this study.

Adrenergic alpha-Agonists↗
PubMed1988

Comparative evaluation of aloe vera in the management of burn wounds in guinea pigs.

An experimental study was designed using Hartley guinea pigs, who received full-thickness burns covering 3 percent of their body surface area by direct contact with a hot plate. A total of 40 animals were equally divided among four modalities of closed burn wound management as follows: group I: silver sulfadiazine (Silvadine); group II: aloe vera gel extract (Carrington Dermal Wound Gel); group III: salicylic acid cream (aspirin); and group IV: plain gauze occlusive dressing only. The dressings were changed daily, and the size and appearance of each burn wound were recorded until complete healing. On the sixth postburn day, quantitative burn wound cultures were made. The average time to complete healing in the control group was 50 days, and the only significant difference was found in the aloe vera-treated animals, which healed on an average of 30 days (p less than 0.02). Wound bacterial counts were effectively decreased by silver sulfadiazine (p = 0.015) and by aloe vera extract (p = 0.015). From our data it appears that aloe gel extracts permit a faster healing of burn wounds.

Administration, Topical↗
PubMed1989

Processed Aloe vera administered topically inhibits inflammation.

Aloe vera preparations were evaluated for topical anti-inflammatory activity using the croton oil-induced edema assay. The results show that small amounts of A. vera given topically will inhibit inflammation induced by a moderate amount of irritant. In general, the decolorized Aloe was more effective than the colorized Aloe (with anthraquinone). A 47.1% inhibition of inflammation was obtained by 5% decolorized irradiated Aloe. These results may be used as a baseline to assess the biologic activity of A. vera in the treatment of inflammation by podiatric physicians.

Administration, Topical↗
PubMed1991

Aloe vera dermal wound gel is associated with a delay in wound healing.

We evaluated the time interval required for wound healing using a standard wound management protocol with and without aloe vera gel. Twenty-one women were studied who had wound complications requiring healing by second intention after cesarean delivery or laparotomy for gynecologic surgery. Wounds treated with standard management healed in a mean (+/- SD) time interval of 53 +/- 24 days, whereas those treated with aloe vera gel required 83 +/- 28 days (P = .003). The use of aloe vera dermal wound gel was associated with a significant delay in wound healing compared with treatment with an otherwise identical regimen that did not include aloe vera.

Adult↗
PubMed1987

Effects of topical ALO 2145 (p-aminoclonidine hydrochloride) on the acute intraocular pressure rise after argon laser iridotomy.

A prospective, randomized, double-masked pilot study compared topical 1% ALO 2145 (p-aminoclonidine hydrochloride, a topical alpha 2-agonist) with a placebo to determine its ability to minimize any acute postoperative intraocular pressure (IOP) increase after argon laser iridotomy. Twenty-eight eyes (21 patients) with chronic narrow angle glaucoma underwent argon laser iridotomy. Fourteen eyes were treated with ALO 2145; the remainder received a placebo. All eyes received one drop of the appropriate medication one hour before and following the iridotomy. Six eyes (43%) treated with the placebo and no eyes treated with ALO 2145 experienced an IOP increase greater than 10 mm Hg over baseline. The mean IOPs and mean IOP changes from baseline were significantly lower during the first three postoperative hours in the eyes treated with ALO 2145. No significant difference was noted in the ease of iridotomy formation, rate of iridotomy closure, visual acuity, anterior segment inflammation, or mean heart rate.

Argon↗
PubMed1986

The Aloe vera phenomenon: a review of the properties and modern uses of the leaf parenchyma gel.

The mucilaginous gel from the parenchymatous cells in the leaf pulp of Aloe vera has been used since early times for a host of curative purposes. This gel should be distinguished clearly from the bitter yellow exudate originating from the bundle sheath cells, which is used for its purgative effects. Aloe vera gel has come to play a prominent role as a contemporary folk remedy, and numerous optimistic, and in some cases extravagant, claims have been made for its medicinal properties. Modern clinical use of the gel began in the 1930s, with reports of successful treatment of X-ray and radium burns, which led to further experimental studies using laboratory animals in the following decades. The reports of these experiments and the numerous favourable case histories did not give conclusive evidence, since although positive results were usually described, much of the work suffered from poor experimental design and insufficiently large test samples. In addition some conflicting or inconsistent results were obtained. With the recent resurgence of interest in Aloe vera gel, however, new experimental work has indicated the possibility of distinct physiological effects. Chemical analysis has shown the gel to contain various carbohydrate polymers, notably either glucomannans or pectic acid, along with a range of other organic and inorganic components. Although many physiological properties of the gel have been described, there is no certain correlation between these and the identified gel components.

Aloe↗